Drug addiction, particularly to opioids like morphine, remains a pressing global health issue. Curcumin, a natural flavonoid, holds promise for treating neurological disorders, yet faces challenges, such as poor solubility and limited bioavailability across the blood-brain barrier. Solid lipid nanoparticles offer a solution, facilitating drug delivery to the brain. Using the Box-Behnken design, nanoparticles were optimised, yielding particles sized 152 nm, with a polydispersity index of 0.254, and an encapsulation efficiency of 70.74%. These nanoparticles enhance curcumin concentration and retention in brain tissue. Behavioural experiments using the conditioned place preference (CPP) test confirmed curcumin's impact on morphine addiction and its modulation of c-Fos gene expression. Pharmacological network analysis identified potential mechanisms of action, highlighting common targets in calcium and serotonin pathways. Docking simulations showed curcumin's affinity for proteins like 5HT1A, MAO-A, and TRPV1, relevant to addiction pathways. This research underscores the potential of curcumin-loaded solid lipid nanoparticles as a therapeutic approach for combating opioid addiction and neurological disorders.
Cuminum cyminum L. (cumin) essential oil (CEO) possesses documented analgesic and anti-inflammatory properties, but its topical application is limited by volatility, instability and low aqueous solubility. This study aimed to develop a CEO nanoemulgel and evaluate its physicochemical characteristics, dermal safety and antinociceptive/anti-inflammatory effects in rodent models. The optimized formulation exhibited nanometric droplet size, uniform distribution and acceptable physical stability. In a rat skin irritation test, repeated application of the CEO nanoemulgel did not produce visible erythema or edema compared with the gel base. In mice, the formulation increased tail-flick latency and reduced nociceptive behaviors in both phases of the formalin test, and histological analysis revealed attenuated inflammatory cell infiltration. These findings suggest that the CEO nanoemulgel has promising antinociceptive and anti-inflammatory activity and appears to be well tolerated in short-term preclinical models. Further studies, including long-term safety assessment, mechanistic analysis and clinical trials, are required before CEO nanoemulgel can be considered for use in humans.
Statement of problem Denture stomatitis (DS) is a common oral disorder in patients with complete maxillary dentures. Typical treatments such as nystatin or azoles lead to drug resistance after a long period. Several studies have shown the antifungal activity of statins against Candida albicans; however, studies on the antifungal effect of atorvastatin against DS are lacking. Purpose The purpose of this randomized, double-blind controlled trial was to assess the effectiveness of atorvastatin mouthwash against DS. Material and methods Twenty-two participants diagnosed with DS were randomly allocated into 2 groups: 11 in the intervention group (atorvastatin mouthwash) and 11 in the control group (nystatin). Participants were asked to use the mouthwash 3 times a day for 2 weeks. The length and width of the lesions were measured, and the number of colonies were counted on days 1 and 14. Data were analyzed with the Spearman correlation coefficient and the Mann-Whitney, Kruskal Wallis, and Wilcoxon tests (α=.05). Results The number of colonies before and after using a mouthwash was significantly different in the control and intervention groups (P=.005 and P=.003, respectively). The number of colonies in the 2 groups were statistically similar on the first day (P=.809). However, a significant difference was observed between the groups on day 14 (P=.024). The number of colonies in the atorvastatin group decreased more than nystatin, indicating that atorvastatin was more effective. A significant difference among the groups was found in terms of Candida species detected after the intervention (P=.032). Conclusions Atorvastatin was effective in reducing Candida species in participants with DS and can be used as an antifungal agent in treating DS.
PURPOSES:The limitations of current sunscreens in protecting against skin cancer and aging have been acknowledged. The use of Rheum ribes extract, rich in phenolic compounds and with strong antioxidant activity, for sunscreen applications has not been extensively studied. This study aims to develop a sunscreen gel containing Rheum ribes (Rhubarb) root extract-loaded solid lipid nanoparticles (SLNs) and evaluate its sun protection factor (SPF) through in vitro testing. METHODS:Rheum ribes extract-loaded SLNs were manufactured by an emulsification-solvent evaporation method. The impact of glyceryl monostearate (GMS) concentration on SLN size, polydispersity index (PDI), entrapment efficiency (EE), and in vitro drug release was investigated. The optimized formulation was incorporated into a gel base, and its SPF was determined using spectrophotometric techniques. Skin permeation and retention studies, as well as skin irritation and cytotoxicity assessments, were conducted. RESULTS:The optimized extract-loaded SLN formulation exhibited a nano-sized diameter (298.07 ± 14.54 nm), uniform distribution (PDI = 0.308 ± 0.001), high entrapment efficiency (69.18 ± 2.60%), and significant skin permeation (32.03 ± 1.44% after 24 h) and retention (6.42 ± 0.39 mg/cm2 after 24 h). This formulation demonstrated a substantially higher SPF (17.435) than the simple extract gel (SPF = 1.913). All gel preparations were found to be nonirritating and non-cytotoxic. CONCLUSION:This study demonstrates the potential of Rheum ribes extract-loaded SLNs for developing effective and safe sunscreen gels. The optimized nanogel formulation achieved significant SPF enhancement while maintaining skin compatibility, highlighting its promising application in cosmetic sun protection.
Melanoma, the most aggressive skin cancer, requires novel and effective treatment strategies. This study developed an optimized mesoporous silica nanoparticle (MSN)-based system for the delivery of curcumin and quercetin, two polyphenolic compounds with anticancer properties, to enhance their transdermal delivery. MSNs were synthesized using the sol-gel method and optimized via a Box-Behnken design, resulting in nanoparticles with an average size of 172.92 ± 23.74 nm and a polydispersity index (PDI) of 0.291 ± 0.026. Drug entrapment efficiencies were 46.25 ± 3.55
Objective:Paraquat (PQ), a widely used non-selective herbicide, induces severe lung toxicity by promoting cell death and tissue necrosis through the generation of reactive oxygen species (ROS) and free radicals. This study aimed to develop and evaluate novel niosomal nanoparticles (NPs) encapsulating curcumin and piperine to mitigate PQ-induced acute pulmonary toxicity in Balb/c mice. Methods:The NPs were prepared using non-ionic surfactants and cholesterol via the thin film hydration method. Results:Characterization revealed high encapsulation efficiency (>85%), proper particle sizes (264-286 nm), narrow polydispersity index (PDI) (0.19 ± 0.04 to 0.23 ± 0.02), and good stability over 90 days. Thermal analysis confirmed successful encapsulation of curcumin and piperine within the niosomal NPs. In vivo studies showed that PQ exposure significantly elevated ROS, lipid peroxidation (LPO), and protein carbonylation (PC) levels, while reducing glutathione (GSH) levels and impairing mitochondrial function (P < 0.001). However, co-treatment with curcumin- and piperine-loaded niosomal NPs effectively reversed these effects (P < 0.001), improving mitochondrial function. Conclusion:The combined formulation of curcumin and piperine in niosomal NPs offers a promising therapeutic strategy for treating PQ-induced pulmonary toxicity, likely due to enhanced bioavailability and potent antioxidant activity.
Oral candidiasis and its association with dental caries necessitate the development of toothpaste with enhanced antifungal properties, particularly for children at high risk of infection. This study aims to investigate the antifungal efficacy of children's toothpaste incorporating biosynthesized silver nanoparticles (AgNPs) using Feijoa sellowiana. Silver fluoride and Feijoa leaf extract were used for the synthesis of AgNPs. The independent variables were the concentration of AgF, pH of the extract, and temperature. The optimized formula was obtained using Design Expert software and Box-Benken design. The physicochemical properties of AgNPs were evaluated by UV-absorption wavelength measurements, SEM, and TEM analyses. Finally, the powder of optimized AgNPs was added to Colgate Kids Toothpaste (R) and its antifungal effect was evaluated using the standard agar well diffusion method. The optimization process identified an AgF concentration of 8 mM, a pH value of 9.56, and a temperature of 58 C-degrees as influential factors for the formulation. The optimized AgNPs exhibited a size of 42.75 nm, and SEM and TEM analyses confirmed their spherical shape. Both toothpaste formulations, with and without AgNPs, demonstrated antifungal activity. Although the antifungal effect of both toothpaste types against Candida glabrata did not show a significant difference (p > 0.088), the toothpaste containing AgNPs exhibited significantly higher antifungal efficacy against Candida albicans (p < 0.014). In conclusion, the biosynthesis of silver nanoparticles using silver fluoride and Feijoa leaf extract as an eco-friendly approach can effectively enhance the antifungal potency of toothpaste against C. albicans.
For more than a decade, researchers have been working to achieve new strategies and smart targeting drug delivery techniques and technologies to treat breast cancer (BC). Nanotechnology presents a hopeful strategy for targeted drug delivery into the building of new therapeutics using the properties of nanomaterials. Nanoparticles are of high regard in the field of diagnosis and the treatment of cancer. The use of these nanoparticles as an encouraging approach in the treatment of various cancers has drawn the interest of researchers in recent years. In order to achieve the maximum therapeutic effectiveness in the treatment of BC, combination therapy has also been adopted, leading to minimal side effects and thus an enhancement in the quality of life for patients. This review article compares, discusses and criticizes the approaches to treat BC using novel design strategies and smart targeting of site-specific drug delivery systems.
Amifostine is used in chemotherapy and radiotherapy as a cytoprotective adjuvant alongside DNA-binding chemotherapeutic agents. It functions by reducing free radicals and detoxifying harmful metabolites. Methotrexate, as an antimetabolite drug has been considered for treating various cancers and autoimmune diseases. However, the cytotoxic effects of methotrexate extend beyond tumor cells to crucial organs, including the heart. This study applied the HUVEC cell line as a reference in vitro model for researching the characteristics of vascular endothelium and cardiotoxicity. The current study aimed to assess amifostine's potential cytoprotective properties against methotrexate-induced cellular damage. Cytotoxicity was measured using the MTT assay. Apoptotic rates were evaluated by Annexin V-FITC/PI staining via flow cytometry. The genoprotective effect of amifostine was determined using the comet assay. Cells were exposed to various amifostine doses (10-200 μg/mL) and methotrexate (2.5 μM) in pretreatment culture condition. Methotrexate at 2.5 μM revealed cytotoxicity, apoptosis, oxidative stress and genotoxicity while highlighting amifostine's cyto/geno protective properties on HUVECs. Amifostine significantly decreased the levels of ROS and LPO while preserving the status of GSH and SOD activity. Furthermore, it inhibited genotoxicity (tail length, %DNA in tail, and tail moment) in the comet assay. Amifostine markedly attenuated methotrexate-induced apoptotic cell death (early and late apoptotic rates). These findings convey that amifostine can operate as a cytoprotectant agent.
Background Aphthous stomatitis is one of the most common oral mucosal diseases. Due to the commonness of recurrent aphthous stomatitis and considering the anti-inflammatory, analgesic, and tissue regenerative properties of atorvastatin and the lack of a study on the effect of statins on minor recurrent aphthous stomatitis, this study investigates the effect of atorvastatin mucoadhesive tablets as a topical treatment on reduction of symptoms and duration of this disease. Methods This study is a randomized, double-blinded clinical trial. Patients were divided into two groups, atorvastatin and, placebo; each of the patients received three mucoadhesive tablets daily in the morning, noon, and night. Finally, the patients were examined on days 0 (baseline), 3, 5, and 7 to determine the diameter of the inflammatory halo. The VAS scale was used to evaluate pain intensity for up to 7 days after each meal. The data was entered into SPSS 24 software and analyzed. Results The halo diameter did not significantly differ between the two groups on baseline (P > 0.05). However, on the study’s third, fifth, and seventh days, the difference between the two groups was remarkable, so in the atorvastatin group, the size of the lesions decreased in shorter healing time (P < 0.05). In addition, the patient’s pain intensity (VAS) also showed a significant decrease in the atorvastatin group except on the first, second, and seventh days of the study (P < 0.05). Conclusion Atorvastatin mucoadhesive tablets effectively reduce the pain of patients with minor recurrent aphthous stomatitis and reduce the size and healing time of the lesions, so their application should be considered in treating minor recurrent aphthous stomatitis. The present study was approved by the Medical Ethics Committee of Mazandaran University of Medical Sciences with the ethics code IR.MAZUMS.REC.1400.8346. Also, this study received code IRCT20170430033722N4.
Abstract In the current study, an ultrasonic approach (as green method) was utilized to prepared kojic acid niosome (kojisome) which aimed to increase the dermal delivery and improving anti-melanogenesis properties. The study’s findings demonstrated that increasing cholesterol enhanced the mean particle size from 68.333 ± 5.686 nm to 325.000 ± 15.099 nm and entrapment efficiency 0% to 39.341 ± 4.126% of the kojisome. Cholesterol may enhance the number and rigidity of bilayers that induced a size enhancement and entrapment efficiency. The skin permeability test revealed that kojisome gel had more kojic acid in dermal layers (437.563 ± 29.857 μg/cm2 or 16.624 ± 1.379%) than kojic acid plain gel (161.290 ± 14.812 μg/cm2 or 6.128 ± 0.672%). The niosome’s lipophilicity allowed for gradual penetration, possibly due to better contact with the skin layers. Also, the extended-release behavior of improved kojisome exhibited high safety profile and low side effect in In vitro cytotoxicity assay, dermal irritation test, and Histo-pathological evaluation. Furthermore, optimum kojisome inhibited melanin formation (53.093 ± 2.985% at 1000 µM) higher than free kojic acid (62.383 ± 1.958%) significantly (p < 0.05). In addition, Kojisome 6 inhibited L-dopa auto-oxidation greater extent (94.806 ± 2.411%) than pure kojic acid solution (72.953 ± 2.728%). Kojisome by delivering and targeting large amount of kojic acid on specific site causes high efficacy in inhibition of melanin synthesis. The observations of this study revealed that the produced kojisome might be used as a potential nano-vehicle for kojic acid dermal administration, thereby opening up innovative options for the treatment of hyperpigmentation problems. Graphical abstract
This study reports on the synthesis of Mn1 - xZnxFe2O4 (Mn, Zn ferrite) magnetic nanoparticles (MNPs) as drug delivery carriers for effective therapeutic outcomes. The MNPs were prepared using the coprecipitation method, and their magnetic properties were investigated based on their composition. Among the compositions tested, Mn0.8Zn0.2Fe2O4 MNPs exhibited superparamagnetic properties with a saturation magnetization moment of 34.6 emu/g at room temperature (25°C). To enhance the water solubility of curcumin (Cur), known for its hydrophobic nature, it was successfully loaded onto alginate (Alg)/chitosan (Chit)@Mn0.8Zn0.2Fe2O4 nanoparticles (NPs). The nanocomposite was characterized by field emission scanning electron microscopy (FE-SEM) which revealed a particle size of approximately 20 nm. The crystalline structure of the NPs was analyzed using X-ray diffraction, while Fourier-transform infrared (FTIR), energy-dispersive X-ray, and map analysis techniques were employed for further characterization. In terms of drug release, there was an initial burst release of Cur (around 18%) within the first hour, followed by a slower release (approximately 61%) over the next 36 h. The anti-tumor properties of the Cur-loaded NPs were evaluated using the Methyl Thiazol Tetrazolium (MTT) assay and quantitative real-time polymerase chain reaction. The MTT assay confirmed a higher cytotoxic effect of Cur-loaded Alg/Chit@Mn0.8Zn0.2Fe2O4 NPs on the MCF-7 breast cancer cell line compared to free Cur, highlighting the significance of incorporating Cur into nano-sized carrier systems.
Metformin is a multipotential compound for treating diabetes II and controlling hormonal acne and skin cancer. This study was designed to enhance metformin skin penetration in melanoma using nanoparticles containing biocompatible polymers. Formulations with various concentrations of chitosan, hyaluronic acid, and sodium tripolyphosphate were fabricated using an ionic gelation technique tailored by the Box-Behnken design. The optimal formulation was selected based on the smallest particle size and the highest entrapment efficiency (EE%) and used in ex vivo skin penetration study. In vitro antiproliferation activity and apoptotic effects of formulations were evaluated using MTT and flow cytometric assays, respectively. The optimized formulation had an average size, zeta potential, EE%, and polydispersity index of 329 ± 6.30 nm, 21.94 ± 0.05 mV, 64.71 ± 6.12%, and 0.272 ± 0.010, respectively. The release profile of the optimized formulation displayed a biphasic trend, characterized by an early burst release, continued by a slow and sustained release compared to free metformin. The ex vivo skin absorption exhibited 1142.5 ± 156.3 μg/cm2 of metformin deposited in the skin layers for the optimized formulation compared to 603.2 ± 93.1 μg/cm2 for the free metformin. Differential scanning calorimetry confirmed the deformation of the drug from the crystal structure to an amorphous state. The attenuated total reflection Fourier transform infrared results approved no chemical interaction between the drug and other ingredients of the formulations. According to the MTT assay, metformin in nanoformulation exhibited a higher cytotoxic effect against melanoma cancer cells than free metformin (IC50: 3.94 ± 0.57 mM vs. 7.63 ± 0.26 mM, respectively, P < 0.001). The results proved that the optimized formulation of metformin could efficiently decrease cell proliferation by promoting apoptosis, thus providing a promising strategy for melanoma therapy.
Purposes Calcium channel blockers, such as diltiazem (DLZ), are important drugs for wound repair treatment. This current study used an ultrasonic method to increase the cutaneous delivery of (DLZ) niosomes. Methods The impact of the cholesterol:surfactant ratio on the DLZ-loaded niosome formulations was investigated. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, drug release, skin sensitivity, animal wound repair model, and histopathological assessment were applied to investigate the characteristics, morphology, and therapeutic effectiveness of the DLZ noisome. Results The results showed that changes in the cholesterol:surfactant ratio can influence the zeta potential and the size of the niosome. The maximum entrapment efficiency was observed to be about 94% when the cholesterol content in the formulation was high. The DLZ release studies revealed that the niosomal formulation was released slowly over the course of 24 h. Macroscopic observations of the wound demonstrated that wound closure in the DLZ-niosome-treated group and the commercial brand was equal and higher than in the other groups (gel base, placebo gel, and negative control). Pathological studies described that the wound repair in the DLZ-niosomal gel group was greater than in the other treatment. All the preparations tested for cutaneous irritation on Wistar rats showed the DLZ niosomal gels to be non-irritating. Conclusion The findings of this study revealed that the prepared DLZ-niosome could be used as a possible nano-vesicle for DLZ cutaneous delivery thus potentially opening up new prospects for the treatment of wound disorders.
Background: Recently, niosomes are becoming popular in drug delivery. The current work aimed to investigate the characteristics, cellular safety, and antifungal activity of ketoconazole-loaded niosome (ketosome). Methods: Ultrasonic approach was employed to prepare ketosome including cholesterol, nonionic surfactant and ketoconazole. The size characteristics and morphological features of ketosome and physicochemical properties of ketoconazole in ketosomes were evaluated using dynamic light scattering (DLS), differential scanning calorimetry (DSC), powder x-ray diffractometer (PXRD), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy. Also, the dissolution rate, cellular safety test and antimycotic properties of ketosome were examined. Results: According to the results, the particle size of the ketosome decreased from 491.400±10.622 to 121.300±7.274 nm by the increment of cholesterol. According to further research, changes in the cholesterol:surfactants ratio can modulate the zeta potential from -27.866±1.069 to -12.500±1.153 mV. The highest entrapment of ketoconazole was about 87% when the cholesterol concentration in the ketosome was high. Ketosome with the maximum cholesterol:surfactants ratio showed the fastest drug release. Furthermore, the cell viability assay revealed that the ketosome had lower cytotoxicity in comparison with pure drug. The cell viability of the ketosome was estimated to be about 90% (HGF cell line). The ketosome had a lower MIC than the pure drug when tested against Candida albicans. Conclusion: The results of this study revealed that the optimized ketoconazole-loaded niosome could be used as a possible nanovesicle for ketoconazole drug delivery, potentially opening up new ways for the management of cutaneous candidiasis complaints.
Hollow mesoporous silica nanoparticles (HMSNs) are promising drug carriers due to their large surface area, high porosity, and biocompatibility. In this study, a straightforward and adjustable synthesis strategy was developed for generating HMSNs with tunable hollow cavities and use them to deliver 5-fluorouracil, a common anticancer drug as model drug. This approach involves using solid SiO2 nanoparticles (sSiO2 NPs) and cetyltrimethylammonium bromide (CTAB) as templates. Remarkably, our study introduces the application of I-optimal design to optimize the size of sSiO2 NPs, subsequently impacting the internal cavity diameter and drug loading capacity of the resulting HMSNs. Dynamic light scattering (DLS), field emission scanning electron microscopy (FE-SEM), transmission electron microscopy (TEM), Brunauer Emmett-Teller (BET) analysis, Fourier-transform infrared (FTIR) spectroscopy and in vitro drug release were conducted to characterize the synthesized particles. Moreover, the blood compatibility and cytotoxicity were performed to demonstrate the biocompatibility of as-synthesized HMSNs. Notably, the investigation unveils that both the internal cavity size and shell thickness have discernible effects on drug loading and release behavior. Furthermore, it was observed that HMSNs particle size played a significant role in their hemocompatibility, while confirming that all synthesized HMSNs exhibited appropriate biocompatibility. Overall, these findings highlight the facile control and manipulation of drug loading and release characteristics within HMSNs through tuning the hollow cores. Additionally, these results demonstrate the potential for regulating hemocompatibility, thereby expanding the range of applications for these nanoparticles. This research provides an innovative and versatile methodology for the synthesis of HMSNs, emphasizing their potential application in drug delivery systems.
Background and Purpose: Following traumatic brain injury, inflammation, mitochondrial dysfunction, oxidative stress, ischemia, and energy crisis can cause mortality or long-term morbidity. As an activator of AMP-activated protein kinase, metformin reduces the secondary injuries of traumatic brain injury by compensating for the lack of energy in damaged cells. But the blood-brain barrier prevents a hydrophilic drug such as metformin from penetrating the brain tissue. Solid lipid nanoparticles with their lipid nature can cross the blood-brain barrier and solve this challenge. so This study aimed to investigate the effect of metformin-loaded lipid nanoparticles (NanoMet) for drug delivery to the brain and reduce complications from traumatic brain injury.Method: Different formulations of NanoMet were designed by Box-Behnken, and after formulation, particle size, zeta potential, and entrapment efficiency were investigated. For in vivo study, Male rats were divided into eight groups, and except for the intact and sham groups, the other groups underwent brain trauma by the Marmarou method. After the intervention, the Veterinary Coma Scale, Vestibular Motor function, blood-brain barrier integrity, cerebral edema, level of inflammatory cytokines, and histopathology of brain tissue were assessed.Results: The optimal formula had a size of 282.2 +/- 9.05 nm, a zeta potential of-1.65 +/- 0.33 mV, and entrapment efficiency of 60.61 +/- 6.09% which released the drug in 1400 min. Concentrations of 5 and 10 mg/kg of this formula improved the consequences of trauma. Conclusion: This study showed that nanoparticles could help target drug delivery to the brain and apply the desired result.
Terbinafine (TER) is a promising candidate medication for the topical treatment of fungal infections. However, its solubility in water and skin permeability are limited. To overcome these limitations, a Terbinafine niosome and niosomal gel was developed. The impact of cholesterol:surfactants on terbinafine incorporated niosome (terbinasome) preparations was examined. Differential scanning calorimetry (DSC), photon correlation spectroscopy (PCS), scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy were used to assess the morphological features of terbinasome and the physicochemical characteristics of TER in terbinasome. The obtained results has shown that Chol enhanced the diameter of the terbinasome from 123.20 +/- 2.86 to 701.93 +/- 17.72 nm. The highest encapsulation of terbinafine was estimated to be around 66% due to the cholesterol:surfactants ratio in the terbinasome was 1:3 and 1:6. Additional examination has revealed that changes in the cholesterol:surfactants ratio can result in a change in the PDI value of between 0.421 +/- 0.004 and 0.712 +/- 0.011. The terbinasome gel was prepared and tested for pharmaceutical testing, including pH, viscosity, spreadability, and stability. The percentage of TER dissolution from terbinasome were determined more than 80% and showed quickest drug release. In a cutaneous permeability examination, the quantity of TER in the cutaneous layers and the receiver compartment were higher for the terbinasome gel than for the TER simple gel. The terbinasome's cell viability was around 90% (HFF cell line) and MTT experiment demonstrated that the terbinasome was not cytotoxic. The MIC of the terbinasome was lower than pure drug against Aspergillus, Fusarium, and Trichophyton. The terbinasomal gels were non-irritant (score < 2) in the cutaneous irritation examination performed on Wistar rats. The research suggests that the optimized terbinasome may be used as a nano-vesicle for TER drug administration, hence opening up new possibilities for the treatment of cutaneous infections.
Background: Recently, nanoparticles were widely used in drug delivery. Fluconazole (FLZ) is a lipid-soluble antifungal, which is utilized in treating fungal infections. The current work aimed to investigate the characteristics and antifungal activity of FLZ nanosuspension. Methods: FLZ nanosuspensions were prepared by Ultrasonication (simple and containing polymer). Surfactants in various concentrations were dissolved in the deionized water, and the drug powder was dispersed in the surfactant solution by a high-speed homogenizer to achieve nanosuspension. The polymer was added to the selected formula. FLZ nanosuspension characteristics, including polydispersity, mean particle size, entrapment efficacy, and zeta potential, were assessed. The release profile via dialysis membrane, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (ATR-FTIR), and TEM were performed for nanosuspension evaluation. Antifungal activity against resistant strains of C. albicans was defined according to the CLSI document guideline. To analyze the results, one-way ANOVA was used, followed by Tukey test. Results: The results showed that increased sonication time and hydrophilic-lipophilic balance (HLB) significantly affected particle size reduction. Moreover, modification in the formulation components had a significant effect on the drug release process, furthermore affecting the properties of the nanoparticles. ATR-FTIR showed no chemical interaction between FLZ and formulation components. Compare to FLZ, a significant reduction (p < 0.05) was detected in the MIC values of both FLZ-resistant and FLZ-susceptible strains of C. albicans against FLZ nanosuspension. Conclusion: It can be concluded that the ratio and amount of surfactants, the HLB, and the sonication process have effects on the properties of the nanoparticle’s characteristics, and selected nanoparticles show suitable antifungal effect against resistant strains of C. albicans.
The bioavailability of drugs is dependent on several factors such as solubility and the administration route. A drug with poor aqueous solubility, therefore, poses challenges with regards to its pharmaceutical advance and ultimately its biological usage. Lipid nanoparticles have been used in pharmaceutical science due to their importance in green chemistry. Their biochemical properties as 'green' materials and biochemical processes as 'green' processes mean they can be environmentally sustainable. Generally, lipid nanoparticles can be employed as carriers for both lipophilic and hydrophilic drugs. The proposed administration route for nanoparticles can present advantages and disadvantages which should be considered by a formulator. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are attractive delivery systems because of their ease of manufacture, biocompatibility, biodegradability, and scale-up capacity of formulation constituents. The easy and simple scalability of novel SLNs and nano lipid carriers, along with their various processing procedures, recent developments, limitation and toxicity, formulation optimization and approaches for the manufacture of lipid nanoparticles, lyophilization and drug release are comprehensively discussed in this review. This review also summarizes the research data related to the various preparation methods and excipients used for SLNs and NLCs in recent years.